PROTAC CYP1B1 degrader-2
PROTAC CYP1B1 degrader-2 is a CYP1B1 PROTAC degrader with a DC50 of approximately 0.1 nM. PROTAC CYP1B1 degrader-2 induces ubiquitination and proteasomal degradation of CYP1B1, and forms a ternary complex with VHL ubiquitin ligase and CYP1B1. PROTAC CYP1B1 degrader-2 inhibits P-gp. PROTAC CYP1B1 degrader-2 inhibits FAK/SRC. PROTAC CYP1B1 degrader-2 exhibits anticancer activity against paclitaxel (HY-B0015)-resistant non-small cell lung cancer. PROTAC CYP1B1 degrader-2 can be used in studies related to non-small cell lung cancer.
(Pink: CYP1B1 ligand (HY-159006); Blue: VHL ligand (HY-112078); Black: linker (HY-W007700)).
For research use only. We do not sell to patients.
- CAS No.: 2836297-26-6
- Formula: C49H56ClN7O5S3
- Molecular Weight:954.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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CYP1B1 ~0.1 nM (DC50) |
VHL |
PROTAC CYP1B1 degrader-2 (Compound PV2) (0.1-10000 nM; 1-48 h) potently induces proteasomal degradation of CYP1B1 in A549/Taxol cells, with a DC50 of approximately 0.1 nM; it achieves >90% degradation at a concentration of 10 nM, and nearly complete degradation within 24 h at 10 nM[1].
PROTAC CYP1B1 degrader-2 (0.1-10 nM; 48 h) enhances the sensitivity of A549/Taxol cells to Taxol in a concentration-dependent manner, effectively reverses Taxol resistance, and exhibits stronger potency than the CYP1B1 inhibitor A1[1].
PROTAC CYP1B1 degrader-2 (0.1-10 nM; 48 h) inhibits the migration of A549/Taxol cells in a concentration-dependent manner, with significant effects at concentrations of 1 nM and 10 nM[1].
PROTAC CYP1B1 degrader-2 (0.1-10 nM) inhibits the invasion of A549/Taxol cells, with a significant effect observed at 10 nM[1].
PROTAC CYP1B1 degrader-2 (0.1-10 nM; 3 h) inhibits the efflux function of P-gp in A549/Taxol cells and increases the intracellular accumulation of Rho123[1].
PROTAC CYP1B1 degrader-2 (0.1-10 nM; 24 h) downregulates the FAK/SRC-paxillin pathway in A549/Taxol cells, and inhibits FAK phosphorylation, SRC activity and expression, as well as paxillin expression[1].
PROTAC CYP1B1 degrader-2 (0.1-10 nM; 24 h) inhibits the EMT pathway in A549/Taxol cells by upregulating E-cadherin and downregulating N-cadherin and vimentin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Taxol-resistant human lung carcinoma A549/Taxol cells
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Concentration:0.1-10000 nM (24 h); 10 nM (time-course)
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Incubation Time:1 h, 6 h, 12 h, 24 h, 36 h, 48 h (10 nM); 24 h (0.1-10000 nM)
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Result:Reduced CYP1B1 protein levels by 50% at 0.1 nM after 24 h.
Reduced CYP1B1 protein levels by 60% at 1000 nM after 24 h.
Achieved a DC50 of approximately 0.1 nM after 24 h of treatment.
Induced >90% CYP1B1 degradation at 10 nM after 24 h, with a "hook" effect observed at 100 nM.
Reduced CYP1B1 levels after 1 h of treatment at 10 nM.
Achieved near-complete CYP1B1 degradation by 24 h at 10 nM.
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Cell Line:Taxol-resistant human lung carcinoma A549/Taxol cells
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Concentration:0.1-10 nM
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Incubation Time:24 h
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Result:Inhibited the phosphorylation of FAK without affecting total FAK levels in a concentration-dependent manner.
Inhibited both phosphorylation and total protein levels of SRC in a concentration-dependent manner.
Chemical Information
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CAS No. 2836297-26-6
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Molecular Weight 954.66
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Formula C49H56ClN7O5S3
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SMILES
CC(C)([C@@H](C(N1[C@H](C(N[C@H](C2=CC=C(C3=C(C)N=CS3)C=C2)C)=O)C[C@@H](O)C1)=O)NC(CCCCCCCOC4=CC=CC=C4C5=CSC(C6=CSC(NC7=CC=C(Cl)C=C7)=N6)=N5)=O)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)